Bicyclo 4.4.0 antiviral derivatives
    38.
    发明授权
    Bicyclo 4.4.0 antiviral derivatives 有权
    双酚4.4.0抗病毒衍生物

    公开(公告)号:US07037913B2

    公开(公告)日:2006-05-02

    申请号:US10393030

    申请日:2003-03-20

    IPC分类号: A61K31/497 C07D401/00

    摘要: This invention provides compounds of Formula I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. A is selected from the group consisting of C1-6alkoxy, C1-6alkyl, C3-7cycloalkyl, phenyl, and heteroaryl; wherein said heteroaryl may be monocyclic or bicyclic and may be comprised of three to eleven atoms selected from the group consisting of C, N, NR9, O, and S, and wherein each ring of said phenyl and heteroaryl is optionally substituted with one to five same or different substituents selected from the group consisting of R19–R23;W is O or —NH;T is Z1 is CR1 or N;Z2 is CR2 or N;Z3 is CR3 or N;Z4 is CR4 or N;Z5 is CR5 or N;Z6 is CR6 or N;Z7 is CR7 or N;Z8 is CR8 or N.

    摘要翻译: 本发明提供具有药物和生物影响性质的式I化合物,其药物组合物和使用方法。 特别地,本发明涉及酰胺哌嗪衍生物。 这些化合物具有独特的抗病毒活性,无论是单独使用还是与其他抗病毒药,抗感染剂,免疫调节剂或HIV进入抑制剂组合使用。 更具体地说,本发明涉及艾滋病毒和艾滋病的治疗。 A选自C 1-6 - 烷氧基,C 1-6 - 烷基,C 3-7环烷基,苯基和 - 杂芳基; 其中所述杂芳基可以是单环或双环的,并且可以由选自C,N,NR 9,O和S的3至11个原子组成,并且其中所述苯基和 杂芳基任选被一至五个相同或不同的选自下组的取代基取代:R 20 -R 23; W是O或-NH; T是Z 1是CR 1或N; Z 2是CR 2或N; Z 3是CR 3或N; Z 4是CR 4或N; Z 5是CR 5或N; Z 6是CR 6或N; N是7或N; Z 8是CR 8或N.

    Indole, azaindole and related heterocyclic amidopiperazine derivatives
    39.
    发明授权
    Indole, azaindole and related heterocyclic amidopiperazine derivatives 有权
    吲哚,氮杂吲哚和相关的杂环酰胺基哌嗪衍生物

    公开(公告)号:US06825201B2

    公开(公告)日:2004-11-30

    申请号:US10127256

    申请日:2002-04-22

    IPC分类号: A61K31496

    摘要: The invention comprises substituted indole, azaindole and related heterocyclic amidopiperazine derivatives of general Formula I wherein: Q is —may represent a bond; A is selected from the group consisting of C1-6alkoxy, C1-6alkyl, C3-7cycloalkyl, phenyl, and heteroaryl; wherein said heteroaryl may be monocyclic or bicyclic and may be comprised of three to eleven atoms selected from the group consisting of C, N, NR9, O, and S, and wherein each ring of said phenyl and heteroaryl is optionally substituted with one to five same or different substituents selected from the group consisting of R19-R23; T is U is NR7, O, or S; V is C(H)kR1, O or N(R7′)k; W is CR3 or NR10; X is CR4 or NR10; Y is CR5 or NR10; Z is CR6 or NR10; k is 0 or 1; and m, n, and p are each independently 0, 1, or 2 provided that the sum of m, n, and p must equal 1 or 2; compositions thereof and their use as antiviral agents, particularly for treating HIV infection.

    摘要翻译: 本发明包括取代的吲哚,氮杂吲哚和通式I的相关杂环酰胺基哌嗪衍生物,其中Q可以表示键; A选自C1-6烷氧基,C1-6烷基,C3-7环烷基,苯基和杂芳基; 其中所述杂芳基可以是单环或双环的,并且可以由选自C,N,NR 9,O和S的三至十一个原子组成,并且其中所述苯基和杂芳基的每个环任选被 一至五个相同或不同的选自R 19 -R 23的取代基; T是U是NR 7,O或S; V是C(H)k R 1,O或N (R 7')k; W是CR 3或NR 10; X是CR 4或NR 10; Y是CR 5或NR 10; Z是CR 6 >或NR 10; k为0或1; m,n和p各自独立地为0,1或2,条件是m,n和p之和必须等于1或2;其组成及其组成 用作抗病毒剂,特别是用于治疗HIV感染。